Short communicationSerotonin modulates the dissociation of [3H]imipramine from human platelet recognition sites
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2019, NeuropharmacologyCitation Excerpt :A low-affinity secondary binding site, termed S2, has been detected in a vestibule extracellular to the S1 site. Several drugs that target SERT display allosteric effects on the high affinity binding of antidepressants as can be assessed by their ability to impair the dissociation of pre-bound radiolabeled inhibitors (Plenge and Mellerup, 1985; Plenge et al., 1991, 2012; Wennogle and Meyerson, 1982). Such compounds include selective serotonin reuptake inhibitors (SSRIs) (citalopram, fluoxetine, sertraline, and paroxetine), tricyclic antidepressants (TCAs) (imipramine and clomipramine), and the endogenous substrate 5-HT.
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2015, Biochimica et Biophysica Acta - General SubjectsCitation Excerpt :Also in the SERT it has been shown that 5-HT can inhibit the dissociation of bound imipramine. If imipramine binds to S1 in SERT this suggests that 5-HT can bind to an additional allosteric site, at least in the presence of a pre-bound imipramine [93]. The LeuT has so far proven to be an excellent model for the mammalian NSS proteins.